Bioactivity | BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research[1]. |
Invitro | BBDDL2059 (Compound 16) (0-65 nM;6 天) 抑制 KARPAS-422 和 Pfeiffer 细胞生长[1]。BBDDL2059 (0-1 μM;48-96 小时) 抑制 EZH2 酶活性,并在清洗后维持对 EZH2 的长期抑制[1]。 Cell Proliferation Assay[1] Cell Line: |
In Vivo | BBDDL2059 (Compound 16) (静脉注射 3 mg/kg,口服 10 mg/kg) 在大鼠中显示 T1/2 为 0.28 小时 (静脉注射),口服生物利用度 (F%) 为 0.05%[1]。 Pharmacokinetic parameters for BBDDL2059 (Compound 16) in rats[1]Route |
Name | BBDDL2059 |
CAS | 2691174-27-1 |
Formula | C27H36N4O4S |
Molar Mass | 512.66 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zhang Y, et.al. Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2. J Med Chem. 2023 Jun 8;66(11):7629-7644. |